2010 Proceedings of the Fall International Convention of The Pharmaceutical Society of Korea

Citation

, 169-169

Abstract

5-HT receptor is widely distributed in the central and peripheral nervous system in mammals. 5HT2C receptor among fourteen 5-HT subtypes plays important roles in several disorders such as depression, anxiety, epilepsy, schizophrenia and sleep disorders. 5-HT2C agonists have been reported to exert selective anti-obesity effects. However, the limit to the development of anti-obesity drugs up to present does not possess good selectivity and specificity of drug candidates to the 5-HT2C receptor. Therefore, anti-obesity drug candidates are greatly focused on developing more selective and specific 5-HT2C agonists.
We chemically synthesized KOPC10 (KP10; the chemical structure is not shown due to patent submission), a selective 5-HT2C agonist, with the purpose of developing therapeutic agents for the treatment of obesity. Pharmacokinetic data of KP10 is not available yet and required for further progress of the drug development steps. The purpose of the study is to investigate pharmacokinetic parameters and bioavailability of a newly synthesized selective agonist of 5-HT2C receptor, KOPC-200105 (KP10) in rats after intravenous and oral administration for the development of therapeutic anti-obesity agents.